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公开(公告)号：US5153226A
公开(公告)日：1992-10-06
申请号：US557204
申请日：1990-07-30
IPC分类号： A61K31/16 , A61K31/165 , A61K31/19 , A61K31/235 , A61K31/27 , A61K31/403 , A61K31/404 , A61K31/405 , A61P3/06 , A61P9/10 , C07C233/07 , C07C233/11 , C07C237/04 , C07C237/06 , C07C237/08 , C07C237/12 , C07C237/20 , C07C237/22 , C07C237/24 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/50 , C07C311/19 , C07C323/60 , C07C335/12 , C07C335/18 , C07C335/20 , C07D209/20 , C07D213/40 , C07D213/56 , C07D295/26 , C07D333/24
CPC分类号： C07D295/26 , C07C233/07 , C07C233/11 , C07C237/04 , C07C237/20 , C07C237/22 , C07C237/24 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/50 , C07C311/19 , C07C323/60 , C07C335/12 , C07C335/18 , C07C335/20 , C07D209/20 , C07D213/56 , C07D333/24 , C07C2101/08 , C07C2103/18
摘要： The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase: ##STR1## wherein R is phenyl or 1- or 2-naphthyl which are unsubstituted or may be substituted; R.sub.1 is hydrogen or a straight or branched alkyl group having from 1 to 6 carbon atoms; R.sub.2 is hydrogen, an aliphatic group, an aromatic group, an aralkyl or diarylalkyl group or R.sub.1 and R.sub.2 form a carbocyclic group; R.sub.3 is hydrogen, an aliphatic group, an aralkyl group wherein the alkyl moiety may contain a carbocyclic entity; R.sub.4 is hydrogen, an aliphatic group, SO.sub.2 R.sub.14, --C(.dbd.S)NHR.sub.15, --CO.sub.2 R.sub.15, --COR.sub.18, or --C(.dbd.O)NHR.sub.15 wherein R.sub.14 is morpholino, phenyl or substituted phenyl; R.sub.15 is an alkyl group, phenyl or phenylalkyl wherein the phenyl group may be substituted; and R.sub.18 is the same is R.sub.15 or is halo-substituted alkyl, 9-fluoroenylmethylene or pyrrolidino.
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公开(公告)号：US5024994A
公开(公告)日：1991-06-18
申请号：US233320
申请日：1988-08-17
申请人： Annette M. Doherty , James P. Hudspeth , James S. Kaltenbronn , Joseph T. Repine , William H. Roark , Ila Sircar , Francis J. Tinney
发明人： Annette M. Doherty , James P. Hudspeth , James S. Kaltenbronn , Joseph T. Repine , William H. Roark , Ila Sircar , Francis J. Tinney
IPC分类号： C07K5/02
CPC分类号： C07K5/0227 , C07K5/0205
摘要： The invention concerns novel renin-inhibitory peptides which are useful for treating renin-assocated hypertension, hyperaldosteronism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.
摘要翻译： 本发明涉及可用于治疗肾素合成的高血压，醛固酮增多症和充血性心力衰竭的新型肾素抑制肽。 包括肽的制备方法，含有它们的组合物和使用它们的方法。 还包括使用该化合物来确定肾素相关性高血压或醛固酮增多症的存在的诊断方法。
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3.发明申请PYRAZOLYL AND PYRIMIDINYL TRICYCLIC ENONES AS ANTIOXIDANT INFLAMMATION MODULATORS 有权作为抗氧化剂炎症调节剂的吡唑并吡啶并吡啶二酮公开(公告)号：US20120196880A1
公开(公告)日：2012-08-02
申请号：US13330378
申请日：2011-12-19
申请人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
发明人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
IPC分类号： A61K31/416 , C07D401/04 , A61K31/4439 , C07D471/04 , A61P29/00 , C07D239/70 , A61K31/517 , C07D487/04 , A61P9/10 , C07D231/54 , A61K31/437
CPC分类号： C07C255/47 , C07D231/54 , C07D239/70 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D487/04
摘要： Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.
摘要翻译： 本文公开了新型抗氧化剂炎症调节剂，包括下式的那些：其中变量在本文中定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品。 还提供了可用于制备化合物的方法和中间体，以及使用该化合物及其组合物的方法。
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公开(公告)号：US5254589A
公开(公告)日：1993-10-19
申请号：US776112
申请日：1991-10-15
IPC分类号： C07C311/53 , C07C311/55 , A61K31/175
CPC分类号： C07C311/53 , C07C311/55
摘要： A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.
摘要翻译： 降低具有式“IMAGE”的血液胆固醇水平的药学上有用的化合物，其中X是氧或-NH-; Ar是苯基，取代的苯基，萘基或取代的萘基; R1是氢，低级烷基或苄基; 并且R 2是具有5至17个碳原子的直链或支链烷基，其可以在1-碳位上被甲基，乙基，苯基或取代的苯基或具有3至8个碳原子的环烷基取代。
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公开(公告)号：US4895834A
公开(公告)日：1990-01-23
申请号：US113277
申请日：1987-11-02
申请人： James P. Hudspeth , James S. Kaltenbronn , Joseph T. Repine , William H. Roark , Michael A. Stier
发明人： James P. Hudspeth , James S. Kaltenbronn , Joseph T. Repine , William H. Roark , Michael A. Stier
IPC分类号： C07D213/56 , C07D233/54 , C07D233/64 , C07D401/12 , C07K5/08
CPC分类号： C07D233/64 , C07D213/56 , C07D401/12 , Y10S530/86
摘要： The invention concerns novel renin-inhibitory peptides which are useful for treating renin associated hypertension, hyperaldosternoism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic test using the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.
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公开(公告)号：US5593967A
公开(公告)日：1997-01-14
申请号：US41647
申请日：1993-04-01
申请人： David C. Horwell , Edward Roberts , Ann Holmes , Janak K. Padia , William H. Roark , Bruce D. Roth , Bharat K. Trivedi , Jurgen Kleinschroth , David C. Rees , Reginald S. Richardson
发明人： David C. Horwell , Edward Roberts , Ann Holmes , Janak K. Padia , William H. Roark , Bruce D. Roth , Bharat K. Trivedi , Jurgen Kleinschroth , David C. Rees , Reginald S. Richardson
IPC分类号： A61K38/00 , C07D209/14 , C07D209/20 , C07K5/02 , C07K5/065 , C07K5/078 , C07K14/595 , C07D209/18 , C07D217/00
CPC分类号： C07K14/595 , C07D209/14 , C07D209/20 , C07K5/0202 , C07K5/06078 , C07K5/06156 , A61K38/00
摘要： Novel cholecystokinin antagonists useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to the withdrawal from chronic treatment with use of nicotine, diazepam, alcohol, cocaine, coffee, or opioids. The compounds of the invention are also useful in treating and/or preventing panic. Also disclosed are pharmaceutical compositions and methods of treatment using the antagonists as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds in diagnostic compositions.
摘要翻译： 新颖的缩胆囊素拮抗剂可用作治疗肥胖的药物，胃肠胃分泌过多，胃泌素依赖性肿瘤或抗精神病药。 此外，化合物是抗焦虑剂和抗溃疡剂。 它们是用于防止使用尼古丁，地西泮，酒精，可卡因，咖啡或阿片样物质从慢性治疗中撤回的反应的药剂。 本发明的化合物也可用于治疗和/或预防恐慌。 还公开了使用拮抗剂的药物组合物和治疗方法以及制备它们的方法和可用于其制备的新型中间体。 本发明的另一个特征是本发明化合物在诊断组合物中的用途。
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公开(公告)号：US5571825A
公开(公告)日：1996-11-05
申请号：US414394
申请日：1995-03-31
申请人： Diane H. Boschelli , David T. Connor , Richard D. Dyer , Sonya S. Khatana , James B. Kramer , William H. Roark
发明人： Diane H. Boschelli , David T. Connor , Richard D. Dyer , Sonya S. Khatana , James B. Kramer , William H. Roark
IPC分类号： A61K31/216 , A61K31/341 , A61K31/352 , A61K31/381 , A61K31/382 , A61K31/444 , A61K31/44 , A61K31/215 , A61K31/235 , A61K31/24 , A61K31/34 , A61K31/35 , A61K31/38
CPC分类号： A61K31/444 , A61K31/216 , A61K31/341 , A61K31/352 , A61K31/381 , A61K31/382
摘要： The present invention provides a method of selectively inhibiting prostaglandin G/H synthase-2 that comprises administering to a patient in need of such inhibition an inhibiting amount of a compound having the Formula I, II or III ##STR1## wherein the R groups and heterocycles are defined in the disclosure.
摘要翻译： 本发明提供了选择性抑制前列腺素G / H合酶-2的方法，其包括向需要这种抑制的患者施用抑制量的具有式I，II或III的化合物， 其中R基团和杂环在本公开内容中定义。
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公开(公告)号：US08513436B2
公开(公告)日：2013-08-20
申请号：US13330378
申请日：2011-12-19
申请人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
发明人： Eric Anderson , Gary L. Bolton , Bradley Caprathe , Xin Jiang , Chitase Lee , William H. Roark , Melean Visnick
IPC分类号： C07D487/00 , C07D239/70 , C07D271/06 , C07D271/10 , C07D261/02 , C07D257/04
CPC分类号： C07C255/47 , C07D231/54 , C07D239/70 , C07D401/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D487/04
摘要： Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.
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